TPX-0005

Catalog No.S8583

TPX-0005 Chemical Structure

Molecular Weight(MW): 355.37

TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).

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Biological Activity

Description TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
Targets
WT ALK [1]
(Cell-free assay)		 ALK(L1196M) [1]
(Cell-free assay)		 ALK(G1202R) [1]
(Cell-free assay)		 Src [1]
(Cell-free assay)
1.01 nM 1.08 nM 1.26 nM 5.3 nM
In vitro

TPX-0005 is an orally available and potent ATP-competitive inhibitor against ALK, ROS1, TRKA, TRKB and TRKC recombinant kinases and their corresponding clinical resistant mutants. TPX-0005 demonstrates potent anti-proliferative activity in the range of sub-nanomolar to low nanomolar in a number of human cancer cell lines and engineered stable cell lines expressing the targeted oncogenes or their solvent front mutants, accompanied by inhibition of target phosphorylation and concomitant inactivation of downstream effectors such as ERK, AKT and STAT3[2]. TPX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib. TPX-0005 is able to not only inhibit the wild-type and a broad spectrum of mutant ALKs, but also overcome primary resistance and suppress metastatic features by inhibiting SRC[1].

In vivo In patient derived xenograft tumor models, TPX-0005 treatment results in significant regression of tumors harboring the oncogenic ALK, ROS1 and TRKC fusions. Moreover, in a series of mouse xenograft tumor models, TPX-0005 exhibits marked anti-tumor activity not only in tumors harboring the wildtype oncogenic targets but also in tumors harboring the oncogenes with the solvent front mutations via inhibition of the target phosphorylation[2].

Protocol

Solubility (25°C)

In vitro DMSO 70 mg/mL (196.97 mM)
Ethanol 10 mg/mL (28.13 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 355.37
Formula

C18H18FN5O2
CAS No. 1802220-02-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03093116 Recruiting Locally Advanced Solid Tumors|Metastatic Solid Tumors|Non Hodgkin Lymphoma TP Therapeutics Inc. February 27 2017 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID